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Medicinal-Pharmaceutical Chemistry Commons™
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- (β-Halo)vinylsulfone (1)
- Alzheimer’s disease (1)
- Arsinothricin (1)
- Binding interface (1)
- Casenilin (1)
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- Circular dichroism (1)
- Computational MD simulation (1)
- DREAM (1)
- Drug discovery (1)
- Dynamics network analysis (1)
- Fluorescence spectroscopy (1)
- Isothermal titration calorimetry (1)
- KChIP3 (1)
- Pain modulation (1)
- Photothermal spectroscopy (1)
- Polyaromatic Hydrocarbons (1)
- Presenilin (1)
- Purine Nucleosides (1)
- Β-Ketosulfone (1)
Articles 1 - 2 of 2
Full-Text Articles in Medicinal-Pharmaceutical Chemistry
Purine Nucleosides Modified At C8 Or C2 Position With (Β-Halo)Vinylsulfone And Β-Ketosulfone Reactive Groups And Their Incorporation Into Dna: Synthesis Of The Organoarsenical Antibiotic Arsinothricin And Polyaromatic Hydrocarbons, Md Abu Hasan Howlader
FIU Electronic Theses and Dissertations
Modified nucleosides gained great attention as potential anticancer and antiviral therapeutics. In this dissertation, synthesis and reactivity of (β-iodovinyl)sulfone and β-ketosulfone groups incorporated into purine nucleosides at C8 or C2 positions and DNA incorporation of their 5' triphosphates have been developed. Moreover, synthesis of novel antibiotic arsinothricin (AST) as well as polycyclic aromatic hydrocarbons (PAHs) have been discussed. The 8-(1-iodo-2-tosylvinyl)-2'-deoxyadenosine and 8-(1-Iodo-2-tosylvinyl)adenosine were synthesized employing iodovinylsulfonation of 8-ethynyl precursors with TsNa/I2/NaOAc. The 8-(β-iodovinyl)sulfonyl-2'-deoxyguanosine was prepared via radical mediated iodovinylsulfonation of 8-ethynyl-2'-deoxyguanosine with TsNHNH2/KI/(BzO)2. Conformationally different C2 substituted isomeric adenosine analogues were prepared by iodovinylsulfonation …
Conformational Dynamics And Stability Associated With Magnesium Or Calcium Binding To Dream In The Regulation Of Interactions Between Dream And Dna Or Presenilins, Khoa Ngoc Pham
FIU Electronic Theses and Dissertations
Downstream regulatory element antagonist modulator (DREAM) is involved in various interactions with targets both inside and outside of the nucleus. In the cytoplasm, DREAM interacts with the C-terminal fragments of presenilins to facilitate the production of β-amyloid plaques in Alzheimer’s disease. In the nucleus, Ca2+ free DREAM directly binds to specific downstream regulatory elements of prodynorphin/c-fos gene to repress the gene transcription in pain modulation. These interactions are regulated by Ca2+ and/or Mg2+ association at the EF-hands in DREAM. Therefore, understanding the conformational dynamics and stability associated with Ca2+ and/or Mg2+ binding to DREAM …